The immunomodulating properties of arglabin, a sesquiterpene lactone isolated from Artemisia myriantha Wall. (Asteraceae) were investigated using the murine macrophage tumor line J774.1. Arglabin-stimulated macrophages displayed a strong cytotoxic activity and the lowest doses (1.25 micrograms/mL and 0.125 micrograms/mL) induced a significant stimulation of cell mitochondrial metabolism, which correlated with [3H]TdR uptake by J774.1 cells under the same experimental conditions. In addition, the secretion of cytokines involved in host defence mechanisms--IL-1, TNF-alpha, and IL-2--was investigated upon incubation of J774-1 cells with arglabin. Arglabin triggered the production of the three cytokines from J774-1 cells. However, the pattern of cytokine secretion differed to some extent, according to the methodology used for cytokine measurement: either traditional bioassay or specific immunoassay (ELISA). Our data emphasize a possible proliferative effect of arglabin in the traditional bioassays, at least for the highest concentrations used. The results were verified with specific ELISA immunoassays. Using either method, lower concentrations of arglabin (ranging from 12.5 micrograms/mL to 0.125 micrograms/mL) were the most effective in inducing IL-1, TNF-alpha, or IL-2 secretion. In addition, preliminary data on phagocytosis showed that arglabin enhanced the uptake of fluorescent latex beads by J774.1 cells.
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ChemMedChem
June 2024
Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center of Russian Academy of Sciences, Arbuzov Street, 8, Kazan, 420088, Russian Federation.
A general method for chemo- and diastereoselective modification of anticancer natural product arglabin with nitrogen- and carbon-centered pronucleophiles under the influence of nucleophilic phosphine catalysts was developed. The locked s-cis-geometry of α-methylene-γ-butyrolactone moiety of arglabin favors for the additional stabilization of the zwitterionic intermediate by electrostatic interaction between phosphonium and enolate oxygen centers, leading to the unprecedentedly high efficiency of the phosphine-catalyzed Michael additions to this sesquiterpene lactone. Using n-BuP as the catalyst, pyrazole, phthalimide, 2-oxazolidinone, 4-quinazolinone, uracil, thymine, cytosine, and adenine adducts of arglabin were obtained.
View Article and Find Full Text PDFEur J Pharmacol
May 2024
Department of Pharmacology, All India Institute of Medical Sciences, New Delhi, India. Electronic address:
Background: Arglabin is a plant alkaloid (sesquiterpene lactone) that is used as an anticancer drug. It has potential anti-diabetic and anti-atherogenic effects.
Purpose: Arglabin has drawn particular attention because of its therapeutic effects as an anti-inflammatory agent in multiple diseases.
Open Access Maced J Med Sci
February 2023
JSC, International Research and Production Holding "Phytochemistry", Karaganda, Republic of Kazakhstan.
Background: At present, more than 8000 sesquiterpene lactones have been isolated and described from natural sources, a significant part of which has cytotoxicity and antitumor activity. One of the practically available sesquiterpene lactones is arglabin, which, as a renewable material, is used for the synthesis of new compounds. The article presents data on the study of cytotoxicity and antitumor activity of the arglabin and its derivatives using molecular modeling methods and, in the experiment and .
View Article and Find Full Text PDFCurr Top Med Chem
May 2024
Department of Botany, University of Kashmir, Srinagar, Jammu & Kashmir, 190006, India.
Biologically active secondary metabolites, essential oils, and volatile compounds derived from medicinal and aromatic plants play a crucial role in promoting human health. Within the large family Asteraceae, the genus consists of approximately 500 species. species have a rich history in traditional medicine worldwide, offering remedies for a wide range of ailments, such as malaria, jaundice, toothache, gastrointestinal problems, wounds, inflammatory diseases, diarrhoea, menstrual pains, skin disorders, headache, and intestinal parasites.
View Article and Find Full Text PDFExpert Opin Drug Discov
December 2022
Department of Biochemistry and Molecular Genetics, American University of Beirut, Beirut, Lebanon.
Introduction: Sesquiterpene lactones (SLs) are one of the most diverse bioactive secondary metabolites found in plants and exhibit a broad range of therapeutic properties . SLs have been showing promising potential in cancer clinical trials, and the molecular mechanisms underlying their anticancer potential are being uncovered. Recent evidence also points to a potential utility of SLs in cancer prevention.
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